CN1255413C - 作为ampa受体正性调节剂的(吡啶并/噻吩并)-[f]-氧杂吖庚因-5-酮衍生物 - Google Patents
作为ampa受体正性调节剂的(吡啶并/噻吩并)-[f]-氧杂吖庚因-5-酮衍生物 Download PDFInfo
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- CN1255413C CN1255413C CNB028118154A CN02811815A CN1255413C CN 1255413 C CN1255413 C CN 1255413C CN B028118154 A CNB028118154 A CN B028118154A CN 02811815 A CN02811815 A CN 02811815A CN 1255413 C CN1255413 C CN 1255413C
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/14—Ortho-condensed systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/08—Antiepileptics; Anticonvulsants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/32—Alcohol-abuse
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Addiction (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Dermatology (AREA)
- Gynecology & Obstetrics (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Description
化合物 | 10μM下的稳态电流增加% |
(S)-2,3,11,11a-四氢-1H,5H-吡咯并[2,1-c]吡啶并[3,2-f][1,4]-氧杂吖庚因-5-酮* | 22 |
(S)-2,3,10,10a-四氢-1H,5H-吡咯并[2,1-c]噻吩并[2,3-f][1,4]-氧杂吖庚因-5-酮(实施例1) | 32 |
(R)-2,3,10,10a-四氢-1H,5H-吡咯并[2,1-c]噻吩并[2,3-f][1,4]-氧杂吖庚因-5-酮(实施例2A) | 20 |
(S)-8-三氟甲基-2,3,11,11a-四氢-1H,5H-吡咯并[2,1-c]-吡啶并[3,2-f][1,4]氧杂吖庚因-5-酮(实施例2B) | 21 |
(R)-8-三氟甲基-2,3,11,11a-四氢-1H,5H-吡咯并[2,1-c]-吡啶并[3,2-f][1,4]氧杂吖庚因-5-酮(实施例2C) | 19 |
(S)-8-甲基-2,3,11,11a-四氢-1H,5H-吡咯并[2,1-c]吡啶并[3,2-f][1,4]-氧杂吖庚因-5-酮盐酸盐(实施例3) | 12 |
(S)-8-氯-2,3,11,11a-四氢-1H,5H-吡咯并[2,1-c]吡啶并[3,2-f][1,4]-氧杂吖庚因-5-酮(实施例4A) | 16 |
(R)-8-氯-2,3,11,11a-四氢-1H,5H-吡咯并[2,1-c]吡啶并[3,2-f][1,4]-氧杂吖庚因-5-酮(实施例4B) | 29 |
(±)-6,6a,7,8,9,10-六氢-12H-吡啶并[2,1-c]吡啶并[3,2-f][1,4]-氧杂吖庚因-12-酮(实施例4D) | 13 |
(S)-7-氯-2,3,10,10a-四氢-1H,5H-吡咯并[2,1-c]噻吩并[3,2-f][1,4]-氧杂吖庚因-5-酮(实施例5) | 16 |
(R)-7-氯-2,3,10,10a-四氢-1H,5H-吡咯并[2,1-c]噻吩并[3,2-f][1,4]-氧杂吖庚因-5-酮(实施例6A) | 20 |
(S)-8-甲氧基-2,3,11,11a-四氢-1H,5H-吡咯并[2,1-c]吡啶并[3,2-f][1,4]-氧杂吖庚因-5-酮(实施例7) | 22 |
Claims (6)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP01202284.4 | 2001-06-14 | ||
EP01202284 | 2001-06-14 |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN2006100598858A Division CN101029051B (zh) | 2001-06-14 | 2002-06-10 | 作为AMPA受体正性调节剂的(噻吩并)-[f]-氧杂吖庚因-5-酮衍生物 |
Publications (2)
Publication Number | Publication Date |
---|---|
CN1516701A CN1516701A (zh) | 2004-07-28 |
CN1255413C true CN1255413C (zh) | 2006-05-10 |
Family
ID=8180476
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CNB028118154A Expired - Fee Related CN1255413C (zh) | 2001-06-14 | 2002-06-10 | 作为ampa受体正性调节剂的(吡啶并/噻吩并)-[f]-氧杂吖庚因-5-酮衍生物 |
CN2006100598858A Expired - Fee Related CN101029051B (zh) | 2001-06-14 | 2002-06-10 | 作为AMPA受体正性调节剂的(噻吩并)-[f]-氧杂吖庚因-5-酮衍生物 |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN2006100598858A Expired - Fee Related CN101029051B (zh) | 2001-06-14 | 2002-06-10 | 作为AMPA受体正性调节剂的(噻吩并)-[f]-氧杂吖庚因-5-酮衍生物 |
Country Status (25)
Country | Link |
---|---|
US (3) | US7345036B2 (zh) |
EP (1) | EP1446407A2 (zh) |
JP (1) | JP4435562B2 (zh) |
KR (1) | KR100864267B1 (zh) |
CN (2) | CN1255413C (zh) |
AR (1) | AR034482A1 (zh) |
AU (1) | AU2002320841B2 (zh) |
BR (1) | BR0210307A (zh) |
CA (1) | CA2449215C (zh) |
CO (1) | CO5550448A2 (zh) |
CZ (1) | CZ296217B6 (zh) |
EC (1) | ECSP034890A (zh) |
HR (1) | HRP20031013A2 (zh) |
HU (1) | HUP0400196A3 (zh) |
IL (2) | IL158928A0 (zh) |
IS (1) | IS7042A (zh) |
MX (1) | MXPA03011562A (zh) |
NO (1) | NO328710B1 (zh) |
NZ (1) | NZ529671A (zh) |
PE (1) | PE20030271A1 (zh) |
PL (1) | PL367185A1 (zh) |
RU (1) | RU2286347C2 (zh) |
SK (1) | SK287583B6 (zh) |
WO (1) | WO2002102808A2 (zh) |
ZA (1) | ZA200309096B (zh) |
Families Citing this family (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
TW200817385A (en) * | 2006-07-04 | 2008-04-16 | Organon Nv | Heterocyclic derivatives |
FR2964969B1 (fr) * | 2010-09-16 | 2012-08-24 | Servier Lab | Nouveaux derives dihydrobenzoxathiazepines, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
Family Cites Families (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB1238719A (zh) * | 1968-11-01 | 1971-07-07 | ||
NZ255097A (en) | 1992-07-24 | 2001-04-27 | Univ California | Heterocyclic derivatives (such as 1-(1,4-bgenzodioxan-5-ylcarbonyl)-1,2,3,6-tetrahydropyridine) and medicaments that enhance synaptic responses |
ES2159714T3 (es) | 1995-01-06 | 2001-10-16 | Hoffmann La Roche | Hidroximetil-imidazodiazepinas y sus esteres. |
US5650409A (en) * | 1995-06-02 | 1997-07-22 | Cortex Pharmaceuticals, Inc. | Benzoyl piperidines/pyrrolidines for enhancing synaptic response |
US5736543A (en) | 1996-04-03 | 1998-04-07 | The Regents Of The University Of California | Benzoxazines for enhancing synaptic response |
ATE303997T1 (de) | 1997-06-09 | 2005-09-15 | Pfizer Prod Inc | Chinazolin-4-on ampa antagonisten |
US5985871A (en) | 1997-12-24 | 1999-11-16 | Cortex Pharmaceuticals, Inc. | Benzoxazine compounds for enhancing synaptic response |
RU2214405C2 (ru) * | 1998-02-18 | 2003-10-20 | НьюроСёрч А/С | Новые соединения и их применение в качестве положительных модуляторов амра-рецепторов |
US6124278A (en) | 1998-04-03 | 2000-09-26 | The Regents Of The University Of California | Acylbenzoxazines for enhancing synaptic response |
AU777036B2 (en) | 1999-05-12 | 2004-09-30 | Antonio Garofalo | Thiazepine inhibitors of HIV-1 integrase |
TWI232863B (en) | 2001-06-11 | 2005-05-21 | Akzo Nobel Nv | Benzoxazepine derivatives |
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2002
- 2002-06-10 NZ NZ529671A patent/NZ529671A/en unknown
- 2002-06-10 CA CA2449215A patent/CA2449215C/en not_active Expired - Fee Related
- 2002-06-10 CN CNB028118154A patent/CN1255413C/zh not_active Expired - Fee Related
- 2002-06-10 US US10/480,569 patent/US7345036B2/en not_active Expired - Fee Related
- 2002-06-10 EP EP02754652A patent/EP1446407A2/en not_active Withdrawn
- 2002-06-10 CZ CZ20033392A patent/CZ296217B6/cs not_active IP Right Cessation
- 2002-06-10 WO PCT/EP2002/006364 patent/WO2002102808A2/en active IP Right Grant
- 2002-06-10 SK SK1526-2003A patent/SK287583B6/sk not_active IP Right Cessation
- 2002-06-10 AU AU2002320841A patent/AU2002320841B2/en not_active Ceased
- 2002-06-10 KR KR1020037016248A patent/KR100864267B1/ko not_active IP Right Cessation
- 2002-06-10 IL IL15892802A patent/IL158928A0/xx active IP Right Grant
- 2002-06-10 MX MXPA03011562A patent/MXPA03011562A/es active IP Right Grant
- 2002-06-10 JP JP2003506280A patent/JP4435562B2/ja not_active Expired - Fee Related
- 2002-06-10 HU HU0400196A patent/HUP0400196A3/hu unknown
- 2002-06-10 BR BR0210307-9A patent/BR0210307A/pt not_active Application Discontinuation
- 2002-06-10 RU RU2004100702/04A patent/RU2286347C2/ru not_active IP Right Cessation
- 2002-06-10 PL PL02367185A patent/PL367185A1/xx unknown
- 2002-06-10 CN CN2006100598858A patent/CN101029051B/zh not_active Expired - Fee Related
- 2002-06-13 AR ARP020102223A patent/AR034482A1/es unknown
- 2002-06-13 PE PE2002000511A patent/PE20030271A1/es not_active Application Discontinuation
-
2003
- 2003-11-17 IS IS7042A patent/IS7042A/is unknown
- 2003-11-18 IL IL158928A patent/IL158928A/en not_active IP Right Cessation
- 2003-11-21 ZA ZA200309096A patent/ZA200309096B/en unknown
- 2003-12-08 HR HR20031013A patent/HRP20031013A2/hr not_active Application Discontinuation
- 2003-12-11 EC EC2003004890A patent/ECSP034890A/es unknown
- 2003-12-11 NO NO20035523A patent/NO328710B1/no not_active IP Right Cessation
- 2003-12-16 CO CO03109961A patent/CO5550448A2/es not_active Application Discontinuation
-
2008
- 2008-02-01 US US12/024,597 patent/US7566778B2/en not_active Expired - Fee Related
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2009
- 2009-02-20 US US12/389,968 patent/US8034804B2/en not_active Expired - Fee Related
Also Published As
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C14 | Grant of patent or utility model | ||
GR01 | Patent grant | ||
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Owner name: ORGANON NV Free format text: FORMER OWNER: AKZO NOVEL N.V. CORP. Effective date: 20070105 |
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Effective date of registration: 20070105 Address after: Holland Patentee after: Organon NV Address before: Holland Arnhem Patentee before: Akzo Nobel N. V. |
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Owner name: MSD OS CO., LTD. Free format text: FORMER NAME: ORGANON NV |
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Address after: Dutch Oss Patentee after: MSD Oss Bv Address before: Dutch Oss Patentee before: Organon NV |
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